1.Effects of ilexonin A on IL-6 and M-CSF following ballon angioplasty in rabbit common carotid artery
Lihua ZHAO ; Zhangwei LI ; Chuang YANG ; Yaqiu JIANG
Journal of Jilin University(Medicine Edition) 2006;0(01):-
Objective To observe the effects of ilexonin A (IA) on IL-6 and M-CSF following ballon angioplasty in rabbit common carotide artery to provide experimental basis for percutaneous coronary interventions. Methods 30 Japanese rabbits were fed with high cholesterol food for 4 weeks. Then they were divided into three groups randomly. Each group had ten rabbits. ①Control group: the incision was sew directly after right carotide artery of the rabbit was seeked. ②Balloon dilation group:the proximal of the carotide artery was cuted,the ballon was delivered and distended,after it was drawn repeatly,the incision was closed. ③IA therapy group: operation was the same to the balloon dilation group,then IA was administered in vein.All of them were fed with high cholesterol diet for 4 weeks and the blood samples were collected 1 d before the operation and 1 d,1,2,4 weeks after the operation. The serum IL-6 and M-CSF levels were determined with radioimmunoassay.The pathological changes of injuried artery were observed. Results ①The IL-6 level in balloon dilation group was higher than that in IA therapy group after the operation (P
2.Inhibitory effects of amiodarone on simvastatin metabolism in human liver microsomes
CHAO WAN ; Zhangwei JIANG ; Zhu NING ; Yang LING ;
Journal of Geriatric Cardiology 2009;6(2):115-118
Objective To investigate the effects ofamiodarone (AMD) on simvastatin (SV) in human liver microsomes and the possible underlying mechanisms. Methods Time-, NADPH- and concentration-dependent inhibitions were tested in HLM. The logarithm of relative inhibition values was plotted versus preincubation time (0, 5, 10, 15, 20min) for a series concentration of AMD used (0, 2, 5,25, 50 μ mol/L), and the slopes determined by linear regression. These slope values represente the observed inactivation rate constants (kobs). A double-reciprocal plot was then constructed using the reciprocal of the ko~ (y-axis) and the reciprocal of the associated inhibitor concentration (x-axis) to estimate the values ofkinact and K, which were two principal kinetic constants that were specific for mechanism-based inhibition (MBI).drug-drug interactions (DDI) potential was predicted based on in vitro data and by using the in vitro-in vivo extrapolation. Results The time-, concentration- and NADPH-dependent charactga'istics confirmed that when SV was the substrate of CYP3A4, the inhibition of AMD to CYP3A4 is MBI. Kj and kinact value were calculated to be 5.1 μ mol/L and 0.018min-1 The Clint of SV was reduced 2.96-5.63 fold when it was administrated with AMD. Conclusion Based on the results, AMD would inhibit SV metabolism via the mechanism-based manner, which would lead to DDI when they are taken together. Careful clinical observation is recommended when AMD and SV have to be simultaneously prescribed.